| CAS |
No.1088991-73-4 |
| 英文名称 |
Filorexant |
| 分子式 |
C24H25FN4O2 |
| 分子量 |
420.48 |
| 溶解性 |
Soluble in DMSO ≥10mg/mL(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
Off-white to brown Soild |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD28100674 |
| 靶点 |
Orexin Receptor (OX Receptor) |
| 通路 |
GPCR & G Protein;Neuronal Signaling |
| 背景说明 |
Filorexant是一种OX1和OX2受体的强效选择性可逆拮抗剂。 |
| 生物活性 |
Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor([1-2] |
| In Vitro |
In radioligand binding and functional cell based assays Filorexant (MK-6096) demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (170 receptors and enzymes. Filorexant (MK-6096) occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM.[1-2] |
| In Vivo |
Filorexant (MK-6096) dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg).[1-2] |
| 动物实验 |
Animal administration[1]The male Sprague Dawley rats (n = 8/study; age: 3-6 months; weight: 450-600 g) were singly housed with water and food ad libitum and a 12 h light: 12 h dark cycle with lights on at 04:00 and off at 16:00. Sleep studies were conducted to evaluate Filorexant (3 and 10 mg/kg， p.o.)， DORA-22 (10 mg/kg， p.o.) and almorexant (3 and 30 mg/kg， p.o.)， employing a counterbalanced crossover design in which all animals were alternatively treated with drug and vehicle daily for either 3 or 7 consecutive days (for DORA-22 and Filorexant， respectively): 2 baseline days (no dosing)， a 2 day vehicle-only run-in， a 3 or 7-day arm of drug or vehicle followed by 3 or 7 days of conditional crossover. Effects of compound treatments relative to vehicle (20% Vitamin E TPGS， p.o.) were evaluated following administration in the active phase).[1-2] |
| 数据来源文献 |
[1]. Winrow CJ， et al. Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. Neuropharmacology. 2012 Feb;62(2):978-87.
[2]. Coleman PJ， et al. Discovery of [(2R，5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. ChemMedChem. 2012 Mar 5 |
| 规格 |
2mg 5mg 10mg 50mg 100mg |
| 单位 |
瓶 |
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